1. Field of the Invention
This invention relates to a novel triazole derivative, and more specifically to a novel triazole derivative having both excellent antimycotic action and high safety, a pharmaceutical comprising the derivative as an effective ingredient, an intermediate of the derivative and preparation process of the derivative.
2. Description of the Related Art
Mycosis can be classified into two types, that is, superficial mycosis represented by various trichophytosis, marginated eczema, psoriasis, cutaneous candidiasis or the like and deep seated mycosis represented by mycotic meningitis, mycotic infectious disease of respiratory organ, fungemia, mycosis of urinary tract or the like. Of these, deep seated mycosis such as candidiasis or aspergillosis tends to show a marked increase in recent days owing to the frequent use of an anticancer chemotherapeutic agent or immunosuppressive agent or lowering in the bioimmunology due to HIV infection or the like. There is accordingly a demand for a pharmaceutical efficacious against such fungi.
As a pharmaceutical effective against Aspergillus and Candida, Amphotericin B and azole-based compounds such as Fluoonazole and Itraconazole are conventionally known, but the number of such pharmaceuticals is not so many yet. So, more effective mycocides are under research and development. For example, a methanesulfonyl-containing compound (Japanese Patent Application Laid-Open No. 85369/1986, Japanese Patent Application Laid-Open No. 223266/1991 or the like) and a difluoromethylene-containing compound (Japanese Patent Application Laid-Open No. 163374/1984, Japanese Patent Application Laid-Open No. 163269/1993 or the like) are known as an azole-based compound.
Therapeutics for deep seated mycosis which have so far been known each has problems in safety and antimycotic action and is not always effective against Aspergillus or Candida. Accordingly, an object of the present invention is to provide a compound which has strong antimycotic action, is effective against Aspergillus and Candida and has high safety; and a pharmaceutical comprising the compound as an effective ingredient.
With the forgoing in view, the present inventors synthesized a number of triazole derivatives and carried out an investigation on the antimycotic action of these derivatives. As a result, it has been found that a triazole derivative represented by the below-described formula (1) and a salt thereof have excellent antimycotic action against Aspergillus and Candida and at the same time have high safety so that it is useful as a pharmaceutical, leading to the completion of the present invention.